匹可硫酸钠的合成工艺研究  

Study on Synthesis Process of Sodium Picosulfate

作　　者：陈年根[1] 林景美 钟霞[1] 王跃梅 CHEN Nian-gen;LIN Jing-mei;ZHONG Xia;WANG Yue-mei(School of Pharmacy,Hainan Medical University,Hainan Haikou 571199;Hainan Women and Children s Medical Center,Hainan Haikou 570206,China)

机构地区：[1]海南医学院药学院,海南海口571199 [2]海南省妇女儿童医学中心,海南海口570206

出　　处：《广州化工》2022年第5期94-96,共3页GuangZhou Chemical Industry

摘　　要：以苯酚和吡啶-2-甲醛为起始原料,经缩合、磺酸酯化和精制等步骤制备匹可硫酸钠。以36%盐酸和乙酸为催化剂,可大大减少异构体杂质。通过甲醇-乙酸乙酯-乙酸精制,可很好控制中间体中的新杂质。以三氧化硫吡啶复合物为磺化剂,可很好控制未知杂质的产生和无机盐的残留。经乙醇和水精制,所得的API澄清度符合质量标准。该工艺反应条件温和、操作简便,为匹可硫酸钠的合成提供了一种新方法。Sodium picosulfate was synthesized from phenol(2)and pyridine-2-carboxalde-hyde(3)as raw matercial via the condensation, sulfonylation and crystallization, etc. The isomer impurity in the intermediate(4)could be greatly reduced by 36% hydrochloric acid and acetic acid as the catalyzer. And the other impurity could be controlled by the purification of methanol, ethyl acetate and acetic acid. The crude Sodium picosulfate was synthetised by sulfur trioxide pyridine complex. And the unknown impurity and inorganic salt could meet the standard. The obtained API clarity was less than No. 1 standard by ethanol and water. The process was simple and a new choice for the production of Sodium picosulfate.

关 键 词：匹可硫酸钠 便秘 合成工艺 

分 类 号：R914[医药卫生—药物化学]